PROTAC KRAS G12C degrader-1 is a PROTAC-based KRASG12C degrader, with an IC50 of 414 nM for CRBN. PROTAC KRAS G12C degrader-1 induces CRBN/ KRASG12C dimerization and degrades GFP- KRASG12C in reporter cells.

Product information

Molecular Weight: 917.47

Formula: C50H54ClFN8O6

Chemical Name: 4-((12-((4-(4-acryloylpiperazin-1-yl)-6-chloro-8-fluoro-7-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)amino)dodecyl)amino)-2-(2, 6-dioxopiperidin-3-yl)isoindoline-1, 3-dione

Smiles: C=CC(=O)N1CCN(CC1)C1=NC(NCCCCCCCCCCCCNC2=CC=CC3=C2C(=O)N(C2CCC(=O)NC2=O)C3=O)=NC2=C(F)C(=C(Cl)C=C12)C1=CC(O)=CC2=CC=CC=C21

InChiKey: FMYAMLPDKZOVMB-UHFFFAOYSA-N

InChi: InChI=1S/C50H54ClFN8O6/c1-2-41(63)58-24-26-59(27-25-58)46-36-30-37(51)42(35-29-32(61)28-31-16-11-12-17-33(31)35)44(52)45(36)56-50(57-46)54-23-14-10-8-6-4-3-5-7-9-13-22-53-38-19-15-18-34-43(38)49(66)60(48(34)65)39-20-21-40(62)55-47(39)64/h2,11-12,15-19,28-30,39,53,61H,1,3-10,13-14,20-27H2,(H,54,56,57)(H,55,62,64)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

PROTAC KRAS G12C degrader-1 (Compound 12) engages CRBN in cells, bound KRASG12C in vitro, induces CRBN/KRASG12C dimerization, and degrades GFP-KRASG12C in reporter cells in a CRBN-dependent manner.

Products are for research use only. Not for human use.